Novel 1,2,4-oxadiazoles as potent and selective histamine H3 receptor antagonists

Article abstract of DOI:10.1016/0960-894X(96)00122-9

Replacement of the isothiourea moiety of known histamine H₃ antagonists by certain 5-membered heteroaromatic systems can give compounds with an improved activity profile. One of these, 3-[(4-chlorophenyl)methyl]-5-[2-(1H-imidazol-4-yl)ethyl] 1,2,4-oxadiazole (GR175737) is a potent, selective, orally active and centally penetrating H₃ antagonist.